Estrogen receptor-beta agonist diarylpropionitrile counteracts the estrogenic activity of estrogen receptor-alpha agonist propylpyrazole-triol in the mammary gland of ovariectomized Sprague Dawley rats

@article{Song2012EstrogenRA,
  title={Estrogen receptor-beta agonist diarylpropionitrile counteracts the estrogenic activity of estrogen receptor-alpha agonist propylpyrazole-triol in the mammary gland of ovariectomized Sprague Dawley rats},
  author={Xiao-Ming Song and Zhongzong Pan},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2012},
  volume={130},
  pages={26-35}
}
  • Xiao-Ming Song, Z. Pan
  • Published 1 May 2012
  • Biology
  • The Journal of Steroid Biochemistry and Molecular Biology
Effects of agonists for estrogen receptor α and β on ovariectomy-induced lower urinary tract dysfunction in the rat.
TLDR
Reduced voiding efficiency in OVX rats can be reversed by 1-wk drug treatment that selectively targets ERα and reduces AP during EUS bursting and also facilitated bladder storage mechanisms by increasing the volume threshold.
Estrogen receptor beta is a negative regulator of mammary cell proliferation
TLDR
ERβ overexpression significantly decreased mammary cell proliferation rate in both the proestrus and diestrus phases, indicating that ERβ, unlike ERα, is a negative regulator of mammary epithelial cell proliferation.
Estrogen receptor beta binds Sp1 and recruits a corepressor complex to the estrogen receptor alpha gene promoter
TLDR
It is demonstrated that ER beta overex- pression in breast cancer cells decreases cell proliferation and down-regulates ER alpha mRNA and protein content, along with a concomitant repression of estrogen-regulated genes.
Estrogen receptor beta binds Sp1 and recruits a corepressor complex to the estrogen receptor alpha gene promoter
TLDR
Evidence is provided for a novel mechanism by which overexpression of ER beta through NCoR is able to down regulate ER alpha gene expression, thus blocking ER alpha’s driving role on breast cancer cell growth.
The Effect of Structural Diversity on Ligand Specificity and Resulting Signaling Differences of Estrogen Receptor α.
TLDR
It is demonstrated that similar chemicals interact differently with ERα and induce different allosteric effects, which explains the observed regulation diversity.
Role of Sex Hormones and Their Receptors on Gastric Nrf2 and Neuronal Nitric Oxide Function in an Experimental Hyperglycemia Model
TLDR
The data suggest that ER’s can regulate nitrergic function by improving Nrf2/nNOS expression in experimental hyperglycemia.
Role of sex hormones and their receptors on gastric Nrf2 and neuronal nitric oxide synthase function in an experimental hyperglycemia model
TLDR
The data suggest that ER’s can regulate nitrergic function by improving Nrf2/nNOS expression in experimental hyperglycemia.
Agonist activation of estrogen receptor beta (ERβ) sensitizes malignant pleural mesothelioma cells to cisplatin cytotoxicity
TLDR
The data presented suggest that selective targeting of ERβ may be an efficacious stand-alone treatment option and/or become an important add-on to existing malignant mesothelioma therapy.
Estrogenic activities of compound GL-1, isolated from Ganoderma lucidum
TLDR
The results showed that GL-1 has a good binding ability to estrogen receptor β, and has estrogen-like effect, which might be related to secretion of estrogen and expression of ERβ by binding to ERs.
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References

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Response-Specific and Ligand Dose-Dependent Modulation of Estrogen Receptor (ER) α Activity by ERβ in the Uterus
TLDR
Findings with ER subtype-selective ligands indicate that ERalpha is the major regulator of estrogen function in the uterus, but that ERbeta does exert effects on some uterine markers of estrogen action.
Estrogen receptors alfa (ERα) and beta (ERβ) differentially regulate proliferation and apoptosis of the normal murine mammary epithelial cell line HC11
TLDR
In HC11 mammary epithelial cells, ERα drives proliferation in response to E2 while ERβ is growth inhibitory, suggesting that use of ERβ agonists will be a useful addition in treatment of breast cancer, which, at present, is only aimed at inhibition of ERα.
Characterization of the Biological Roles of the Estrogen Receptors, ERα and ERβ, in Estrogen Target Tissues in Vivo through the Use of an ERα-Selective Ligand
TLDR
Propyl pyrazole triol (PPT) was found to be as efficacious as 17α-ethinyl-17β-estradiol in stimulating uterine weight gain and up-regulating complement 3 gene expression and was also effective in the brain.
Hormone replacement therapy with estrogen or estrogen plus medroxyprogesterone acetate is associated with increased epithelial proliferation in the normal postmenopausal breast.
TLDR
It is shown that postmenopausal HRT with E+P was associated with greater breast epithelial cell proliferation and breast epithelium density than E alone or no HRT, and breast proliferation was localized to the terminal duct-lobular unit of the breast, which is the site of development of most breast cancers.
Interaction of Estrogenic Chemicals and Phytoestrogens with Estrogen Receptor β.
TLDR
The estrogenic activity of environmental chemicals and phytoestrogens in competition binding assays with ERα or ERβ protein, and in a transient gene expression assay using cells in which an acute estrogenic response is created by cotransfecting cultures with recombinant human ERβ complementary DNA (cDNA) in the presence of an estrogen-dependent reporter plasmid are investigated.
An estrogen receptor-alpha knock-in mutation provides evidence of ligand-independent signaling and allows modulation of ligand-induced pathways in vivo.
TLDR
The ENERKI phenotype confirmed that ligand-induced activation of ERalpha is crucial in the female reproductive tract and mammary gland development, and hypothesize that ENerKI animals were particularly sensitive to DES-induced inhibition of ER alpha due to up-regulated uterine ERbeta levels.
Evaluation of an Estrogen Receptor-β Agonist in Animal Models of Human Disease
TLDR
It is concluded that ERβ does not mediate the bone-sparing activity of estrogen on the rat skeleton and that it does not affect ovulation or ovariectomy-induced weight gain.
Biological Role of Pituitary Estrogen Receptors ERα and ERβ on Progesterone Receptor Expression and Action and on Gonadotropin and Prolactin Secretion in the Rat
TLDR
The finding that activation of ERβ with its selective DPN agonist had an estrogenic effect on IR-PR nuclei, but not on GnRH self-priming, a characteristic ERα-mediated effect of E, suggests that the biological action of E at the pituitary may involve both isoforms of ER.
Differential regulation of Estrogen Receptor (ER)α and ERβ in primate mammary gland
TLDR
Control of gonadal hormone receptors during the menstrual cycle, pregnancy, and lactation in rhesus monkey mammary gland is reported on and it is found that ERα but not ERβ is down-regulated when E2 levels increase and when cells enter the cell cycle.
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